New FDA Approval: Deucravacitinib (Sotyktu), a First-In-Class Oral, Allosteric Tyrosine Kinase 2 Inhibitor
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While gadolinium-based MRI contrast agents (GBCAs) are important for enhancing MRI and MRA imaging, several studies have shown that gadolinium can be retained in the brain and body for months to years after GBCA injection, prompting the FDA to issue box warnings to the drug class. Gadopiclenol, the ninth approved GBCA, was designed to enable use of a lower gadolinium dose than other agents. This highlight reviews how it works and why it’s notable.
Leniolisib: The First PI3K Inhibitor First Approved Outside of Oncology
Leniolisib is a selective PI3Kδ inhibitor that received approval in March 2023 from the FDA as a first-in-class treatment for activated PI3K-δ syndrome (APDS), a genetic immunodeficiency disorder caused by PI3Kδ activation. The leniolisib discovery program is notable for several reasons: it is a first approval for a PI3K inhibitor outside of oncology; the first approved drug for APDS; has a novel chemotype that appears to avoid safety issues that led to black box warnings seen with other PI3K molecules; and it overcame a polymorph issue with an early lead that led to inconsistent exposures.
Molecules on the Move: April '23
This article compiles 20+ recent small molecules of general interest in the news in April 2023, with structures where they are available. Capacity Bio’s MAS Receptor Agonists with $35M Raised for FIH Clinical Trials MAS modulator from WO2022165189 example 107 New start-up Capacity Bio backed by RA Capital, Insight Partners, and Remiges [...]
Patent Highlights: Allosteric AR Modulators, Glycogen Synthase Inhibitors, and More
This article highlights million-dollar molecules that were recently in the news with related patent applications that give clues to their structures and properties. This edition includes Maze’s glycogen synthase 1 (GYS1) inhibitors that were recently licensed to Sanofi, allosteric androgen receptor (AR) modulators that may be of interest to targeted protein degradation researchers, brain-penetrant HER2 and ROCK2 inhibitors, and MDM2 degraders.
Small Molecules Acquired in 2021 M&A: Deep Dive
There were 16 acquisitions of companies with small molecule drug assets in 2021 and one merger. Here is a more in-depth look into all of the lead small molecules acquired in 2021, including a review of: The lead molecules in each acquisition and their structural representations where disclosed The mechanism of action, stage, and indication of [...]
